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新型1,4 - 二氢吡啶的合成及其降压活性研究,该二氢吡啶在3 - 酯位含有带硝氧基的硝基咪唑基取代基。

Synthesis and antihypertensive activities of new 1,4-dihydropyridine containing nitroimidazolyl substituent with a nitrooxy group at the 3-ester position.

作者信息

Shafiee Abbas, Rastkary Noushin, Jorjani Masoumeh, Shafaghi Bijan

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, P.O. Box: 14155-6451, Tehran, Iran.

出版信息

Arch Pharm (Weinheim). 2002 Mar;335(2-3):69-76. doi: 10.1002/1521-4184(200203)335:2/3<69::AID-ARDP69>3.0.CO;2-8.

Abstract

New analogues of nifedipine, in which the ortho nitrophenyl group of position 4 is replaced by 1-methyl-4-nitro-5-imidazolyl or 1-methyl-5-imidazolyl with a nitrooxy group at the 3-ester position were synthesized, and the antihypertensive activity of the compounds was examined by the tail-cuff method and compared with TNG and nifedipine. Compounds 11g, 11i-11m, 11o, 11r, and 11v showed activity similar to nifedipine and TNG.

摘要

合成了硝苯地平的新类似物,其中4位的邻硝基苯基被1-甲基-4-硝基-5-咪唑基或1-甲基-5-咪唑基取代,且在3-酯位带有硝氧基,并采用尾套法检测了这些化合物的降压活性,并与替米沙坦(TNG)和硝苯地平进行了比较。化合物11g、11i - 11m、11o、11r和11v显示出与硝苯地平和替米沙坦相似的活性。

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